Target type: molecularfunction
Combining with corticotropin-releasing hormone and transmitting the signal to initiate a change in cell activity. [GOC:signaling, ISBN:0838577016, PMID:11027914, PMID:15134857]
Corticotropin-releasing hormone receptor (CRHR) activity is a molecular function that involves the binding of corticotropin-releasing hormone (CRH) to its receptor, initiating a signaling cascade that leads to the release of adrenocorticotropic hormone (ACTH) from the pituitary gland. This process plays a crucial role in the stress response, regulating various physiological and behavioral processes.
CRHRs are G protein-coupled receptors (GPCRs) that are found in various tissues throughout the body, including the brain, pituitary gland, adrenal glands, and immune cells. When CRH binds to its receptor, it triggers a conformational change in the receptor, activating a signaling pathway involving G proteins and downstream effectors.
The activation of CRHRs leads to the production of cAMP (cyclic adenosine monophosphate) and the activation of protein kinase A (PKA). PKA subsequently phosphorylates various proteins involved in the stress response, including transcription factors that regulate the expression of genes involved in the synthesis and release of ACTH.
ACTH, once released from the pituitary gland, travels to the adrenal glands, where it stimulates the production and release of cortisol, the primary stress hormone. Cortisol, in turn, exerts its effects on various organs and tissues, helping to regulate blood glucose levels, blood pressure, and the immune system.
In addition to its role in the stress response, CRHR activity has also been implicated in other physiological processes, including:
- Regulation of mood and behavior
- Appetite regulation
- Energy homeostasis
- Sleep-wake cycles
- Reproductive function
- Immune function
CRHR activity is tightly regulated by a complex interplay of factors, including:
- Levels of CRH in the circulation
- Expression and sensitivity of CRHRs
- Activity of signaling pathways downstream of CRHRs
- Levels of other hormones and neurotransmitters
Dysregulation of CRHR activity has been linked to various disorders, including anxiety disorders, depression, and post-traumatic stress disorder (PTSD). Medications that target CRHRs are currently being investigated as potential treatments for these conditions.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Corticotropin-releasing factor receptor 1 | A corticotropin-releasing factor receptor 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P34998] | Homo sapiens (human) |
| Corticotropin-releasing factor receptor 2 | A corticotropin-releasing factor receptor 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13324] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| hypericin | |||
| palmidrol | palmidrol: a cannabinoid receptor-inactive eCB-related molecule used as prophylactic in helping to prevent respiratory viral infection palmitoyl ethanolamide : An N-(long-chain-acyl)ethanolamine that is the ethanolamide of palmitic (hexadecanoic) acid. | endocannabinoid; N-(long-chain-acyl)ethanolamine; N-(saturated fatty acyl)ethanolamine | anti-inflammatory drug; anticonvulsant; antihypertensive agent; neuroprotective agent |
| nbi 27914 | dialkylarylamine; tertiary amino compound | ||
| antalarmin | antalarmin : A pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidin-4-amine which is substituted by methyl groups at positions 2, 5, and 6, by a mesityl group at position 7, and in which the amino substituent at position 4 has been substituted by ethyl and butyl groups. It is an antagonist of corticotropin-releasing factor 1 (CRF-1) receptors (Ki = 1 nM). | pyrrolopyrimidine; tertiary amino compound | corticotropin-releasing factor receptor antagonist |
| capsaicin | ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers. | capsaicinoid | non-narcotic analgesic; TRPV1 agonist; voltage-gated sodium channel blocker |
| anandamide | anandamide : An N-acylethanolamine 20:4 resulting from the formal condensation of carboxy group of arachidonic acid with the amino group of ethanolamine. | endocannabinoid; N-acylethanolamine 20:4 | human blood serum metabolite; neurotransmitter; vasodilator agent |
| ssr 125543a | SSR125543: a CRF1 receptor antagonist with antidepressant-like effects | amine | |
| n-oleoylethanolamine | N-oleoylethanolamine: ceramidase inhibitor oleoyl ethanolamide : An N-(long-chain-acyl)ethanolamine that is the ethanolamide of oleic acid. The monounsaturated analogue of the endocannabinoid anandamide. | endocannabinoid; N-(long-chain-acyl)ethanolamine; N-acylethanolamine 18:1 | EC 3.5.1.23 (ceramidase) inhibitor; geroprotector; PPARalpha agonist |
| cp 154526 | |||
| ucb 35625 | UCB 35625: J-113863 is the (trans)-isomer; structure in first source | ||
| r 121919 | |||
| pexacerfont | pyrazolopyridine | ||
| 4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)pyrazolo(1,5-a)pyrimidine | 4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)pyrazolo(1,5-a)pyrimidine: an hCRF(1) antagonist; structure in first source | ||
| nbi-34041 | NBI-34041: high-affinity CRF1 (corticotropin-releasing factor receptor 1) receptor antagonist for attenuating elevated stress response | ||
| dmp 696 | DMP 696: a CRF(1) receptor antagonist; structure in first source | ||
| cp 154526 | CP 154526: structure in first source | ||
| gsk 561679 | NBI 77860: a CRF1 receptor antagonist; structure in first source | ||
| bms 665053 | BMS 665053: structure in first source | ||
| nitd 609 | NITD 609: an antimalarial and coccidiostat; structure in first source |